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以牛血清白蛋白为载体,采用高压均质法制备替莫唑胺白蛋白纳米粒,并运用脑微透析技术,考察该纳米粒经大鼠尾静脉注射给药后的脑内递药特性。结果表明,白蛋白纳米粒形态圆整,平均粒径为(117.60±3.40)nm,电位为(-14.70±3.51)mV,包封率与载药量分别为(52.16±2.23)%和(5.33±0.10)%。替莫唑胺白蛋白纳米粒组的tmax和AUC0→t比其溶液剂组显著提高,但cmax无显著差异。结果提示本品可延长药物在脑内的持续时间,促进药物的脑内吸收,有望成为替莫唑胺脑部递药的有效载体。
Using bovine serum albumin as carrier, temozolomide albumin nanoparticles were prepared by high pressure homogenization, and the intracerebral drug delivery characteristics of the nanoparticles were determined by brain microdialysis. The results showed that the morphology of albumin nanoparticles was round with average particle diameter of (117.60 ± 3.40) nm and potential of (-14.70 ± 3.51) mV, encapsulation efficiency and drug loading were (52.16 ± 2.23)% and (5.33 ± 0.10)%. Temozolomide albumin nanoparticles group tmax and AUC0 → t than the solution group significantly increased, but cmax no significant difference. The results suggest that this product can extend the duration of drugs in the brain and promote absorption of the drug in the brain is expected to become an effective carrier of temozolomide brain delivery.